Clinical Applications

The definitive identification of a therapeutic raison d'etre for H3 antagonists will happen in the clinic. A handful of H3 ligands are reported to have entered clinical testing. ABT-834 entered Phase-I trials for the indication of cognitive disorders in May 2003 but no news has been reported since that time. GT-2331 (11) was approved for Phase-II clinical trials in 1999 but no news has been reported since then [4]. At this point, there are no data available to assess the therapeutic potential in human disease (See Table 5.1).

In conclusion, H3 ligands offer the attractive vista of multiple applications in various disorders, but the ultimate definition of their therapeutic utility will have to await clinical trial results. Future work will determine whether inverse agonists, neutral antagonists, or protean agonists will constitute the more useful pharmacological intervention.


Numerous pharmaceutical companies and academic laboratories have published data on a wide variety of small molecule H3 antagonists/inverse agonists. Highlights of the data reported since the last review in this book series [67] will be reported here.

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